alpha-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study

• Type: Article in International Scientific Journal
• Date: 2017

Authors

Proenca, C (Author) Other; Freitas, M (Author) Other; Ribeiro, D (Author) Other; Oliveira, EFT (Author) Other; Sousa, JLC (Author) Other; Tome, SM (Author) Other; Ramos, MJ (Author) FCUP; Silva, AMS (Author) Other; Pedro A Fernandes (Author) FCUP; Eduarda Fernandes (Author) FFUP

Journal

Title: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 32

Pages: 1216-1228

ISSN: 1475-6366

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 246 Citations

Scopus - 282 Citations

Other information

Authenticus ID: P-00N-1YY

DOI: 10.1080/14756366.2017.1368503

Abstract (EN): alpha-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia ( PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of alpha-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A-and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed alpha-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 13